Gilliam Amanda J H, Smith Joshua N, Flather Dylan, Johnston Kevin M, Gansmiller Andrew M, Fishman Dmitry A, Edgar Joshua M, Balk Mark, Majumdar Sudipta, Weiss Gregory A
Department of Chemistry, and ‡Department of Molecular Biology and Biochemistry, University of California , Irvine, California 92697-2025, United States.
J Med Chem. 2016 Apr 28;59(8):4019-25. doi: 10.1021/acs.jmedchem.5b01536. Epub 2016 Apr 11.
Caveolin-1 is a target for academic and pharmaceutical research due to its many cellular roles and associated diseases. We report peptide WL47 (1), a small, high-affinity, selective disrupter of caveolin-1 oligomers. Developed and optimized through screening and analysis of synthetic peptide libraries, ligand 1 has 7500-fold improved affinity compared to its T20 parent ligand and an 80% decrease in sequence length. Ligand 1 will permit targeted study of caveolin-1 function.
由于其多种细胞作用及相关疾病，小窝蛋白-1成为学术和制药研究的一个靶点。我们报告了肽WL47（1），一种小的、高亲和力、选择性破坏小窝蛋白-1寡聚体的物质。通过对合成肽库的筛选和分析开发并优化后，配体1与其T20母体配体相比，亲和力提高了7500倍，序列长度减少了80%。配体1将允许对小窝蛋白-1的功能进行靶向研究。
